Search Results - "Colclough, Nicola"

The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro‑2H‑pyran-4-yl)-1,3-dihydro‑2H‑imidazo[4,5‑c]quinolin-2-one) by Pike, Kurt G, Barlaam, Bernard, Cadogan, Elaine, Campbell, Andrew, Chen, Yingxue, Colclough, Nicola, Davies, Nichola L, de-Almeida, Camila, Degorce, Sebastien L, Didelot, Myriam, Dishington, Allan, Ducray, Richard, Durant, Stephen T, Hassall, Lorraine A, Holmes, Jane, Hughes, Gareth D, MacFaul, Philip A, Mulholland, Keith R, McGuire, Thomas M, Ouvry, Gilles, Pass, Martin, Robb, Graeme, Stratton, Natalie, Wang, Zhenhua, Wilson, Joanne, Zhai, Baochang, Zhao, Kang, Al-Huniti, Nidal

“…ATM inhibitors, such as 7, have demonstrated the antitumor potential of ATM inhibition when combined with DNA double-strand break-inducing agents in mouse…”
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Structure- and Reactivity-Based Development of Covalent Inhibitors of the Activating and Gatekeeper Mutant Forms of the Epidermal Growth Factor Receptor (EGFR) by Ward, Richard A, Anderton, Mark J, Ashton, Susan, Bethel, Paul A, Box, Matthew, Butterworth, Sam, Colclough, Nicola, Chorley, Christopher G, Chuaqui, Claudio, Cross, Darren A. E, Dakin, Les A, Debreczeni, Judit É, Eberlein, Cath, Finlay, M. Raymond V, Hill, George B, Grist, Matthew, Klinowska, Teresa C. M, Lane, Clare, Martin, Scott, Orme, Jonathon P, Smith, Peter, Wang, Fengjiang, Waring, Michael J

“…A novel series of small-molecule inhibitors has been developed to target the double mutant form of the epidermal growth factor receptor (EGFR) tyrosine kinase,…”
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Brain metastatic outgrowth and osimertinib resistance are potentiated by RhoA in EGFR-mutant lung cancer by Adua, Sally J., Arnal-Estapé, Anna, Zhao, Minghui, Qi, Bowen, Liu, Zongzhi Z., Kravitz, Carolyn, Hulme, Heather, Strittmatter, Nicole, López-Giráldez, Francesc, Chande, Sampada, Albert, Alexandra E., Melnick, Mary-Ann, Hu, Bomiao, Politi, Katerina, Chiang, Veronica, Colclough, Nicola, Goodwin, Richard J. A., Cross, Darren, Smith, Paul, Nguyen, Don X.

“…The brain is a major sanctuary site for metastatic cancer cells that evade systemic therapies. Through pre-clinical pharmacological, biological, and molecular…”
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Building on the success of osimertinib: achieving CNS exposure in oncology drug discovery by Colclough, Nicola, Chen, Kan, Johnström, Peter, Fridén, Markus, McGinnity, Dermot F.

“…•Brain malignancies have a poor prognosis and are a significant unmet need.•The blood brain barrier excludes most xenobiotics from the brain, limiting…”
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Further Considerations Towards an Effective and Efficient Oncology Drug Discovery DMPK Strategy by Williamson, Beth, Colclough, Nicola, Fretland, Adrian John, Jones, Barry Christopher, Jones, Rhys Dafydd Owen, McGinnity, Dermot Francis

“…DMPK data and knowledge are critical in maximising the probability of developing successful drugs via the application of in silico, in vitro and in vivo…”
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Matched Molecular Pairs as a Guide in the Optimization of Pharmaceutical Properties; a Study of Aqueous Solubility, Plasma Protein Binding and Oral Exposure by Leach, Andrew G, Jones, Huw D, Cosgrove, David A, Kenny, Peter W, Ruston, Linette, MacFaul, Philip, Wood, J. Matthew, Colclough, Nicola, Law, Brian

“…By identifying every pair of molecules that differ only by a particular, well-defined, structural transformation in a database of measured properties and…”
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Biophysical methods in drug discovery from small molecule to pharmaceutical by Holdgate, Geoffrey, Geschwindner, Stefan, Breeze, Alex, Davies, Gareth, Colclough, Nicola, Temesi, David, Ward, Lara

“…Biophysical methods have become established in many areas of drug discovery. Application of these methods was once restricted to a relatively small number of…”
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A combined spectroscopic and crystallographic approach to probing drug–human serum albumin interactions by Buttar, David, Colclough, Nicola, Gerhardt, Stefan, MacFaul, Philip A., Phillips, Scott D., Plowright, Alleyn, Whittamore, Paul, Tam, Kin, Maskos, Klaus, Steinbacher, Stefan, Steuber, Holger

“…The displacement of probes that bind selectively to subdomains IIA or IIIA on human serum albumin (HSA) by competing compounds has been followed using…”
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Expanding the Armory: Predicting and Tuning Covalent Warhead Reactivity by Lonsdale, Richard, Burgess, Jonathan, Colclough, Nicola, Davies, Nichola L, Lenz, Eva M, Orton, Alexandra L, Ward, Richard A

“…Targeted covalent inhibition is an established approach for increasing the potency and selectivity of potential drug candidates, as well as identifying potent…”
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Unbound Brain-to-Plasma Partition Coefficient, Kp,uu,brain—a Game Changing Parameter for CNS Drug Discovery and Development by Loryan, Irena, Reichel, Andreas, Feng, Bo, Bundgaard, Christoffer, Shaffer, Christopher, Kalvass, Cory, Bednarczyk, Dallas, Morrison, Denise, Lesuisse, Dominique, Hoppe, Edmund, Terstappen, Georg C., Fischer, Holger, Di, Li, Colclough, Nicola, Summerfield, Scott, Buckley, Stephen T., Maurer, Tristan S., Fridén, Markus

“…Purpose More than 15 years have passed since the first description of the unbound brain-to-plasma partition coefficient (K p,uu,brain ) by Prof. Margareta…”
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Discovery of a Potent and Selective EGFR Inhibitor (AZD9291) of Both Sensitizing and T790M Resistance Mutations That Spares the Wild Type Form of the Receptor by Finlay, M. Raymond V, Anderton, Mark, Ashton, Susan, Ballard, Peter, Bethel, Paul A, Box, Matthew R, Bradbury, Robert H, Brown, Simon J, Butterworth, Sam, Campbell, Andrew, Chorley, Christopher, Colclough, Nicola, Cross, Darren A. E, Currie, Gordon S, Grist, Matthew, Hassall, Lorraine, Hill, George B, James, Daniel, James, Michael, Kemmitt, Paul, Klinowska, Teresa, Lamont, Gillian, Lamont, Scott G, Martin, Nathaniel, McFarland, Heather L, Mellor, Martine J, Orme, Jonathon P, Perkins, David, Perkins, Paula, Richmond, Graham, Smith, Peter, Ward, Richard A, Waring, Michael J, Whittaker, David, Wells, Stuart, Wrigley, Gail L

“…Epidermal growth factor receptor (EGFR) inhibitors have been used clinically in the treatment of non-small-cell lung cancer (NSCLC) patients harboring…”
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Preclinical Comparison of the Blood-brain barrier Permeability of Osimertinib with Other EGFR TKIs by Colclough, Nicola, Chen, Kan, Johnström, Peter, Strittmatter, Nicole, Yan, Yumei, Wrigley, Gail L, Schou, Magnus, Goodwin, Richard, Varnäs, Katarina, Adua, Sally J, Zhao, Minghui, Nguyen, Don X, Maglennon, Gareth, Barton, Peter, Atkinson, James, Zhang, Lin, Janefeldt, Annika, Wilson, Joanne, Smith, Aaron, Takano, Akihiro, Arakawa, Ryosuke, Kondrashov, Mikhail, Malmquist, Jonas, Revunov, Evgeny, Vazquez-Romero, Ana, Moein, Mohammad Mahdi, Windhorst, Albert D, Karp, Natasha A, Finlay, M Raymond V, Ward, Richard A, Yates, James W T, Smith, Paul D, Farde, Lars, Cheng, Zack, Cross, Darren A E

“…Osimertinib is a potent and selective EGFR tyrosine kinase inhibitor (EGFR-TKI) of both sensitizing and T790M resistance mutations. To treat metastatic brain…”
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Gradient elution in counter-current chromatography: A new layout for an old path by Ignatova, Svetlana, Sumner, Neil, Colclough, Nicola, Sutherland, Ian

“…Gradient elution in CCC is a powerful tool, which needs further systematic development to become robust and easy to use. The first attempt to build a…”
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An Investigation into the Prediction of in Vivo Clearance for a Range of Flavin-containing Monooxygenase Substrates by Jones, Barry C, Srivastava, Abhishek, Colclough, Nicola, Wilson, Joanne, Reddy, Venkatesh Pilla, Amberntsson, Sara, Li, Danxi

“…Flavin-containing monooxygenases (FMO) are metabolic enzymes mediating the oxygenation of nucleophilic atoms such as nitrogen, sulfur, phosphorus, and…”
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Discovery and Optimization of Potent, Efficacious and Selective Inhibitors Targeting EGFR Exon20 Insertion Mutations by Thomson, Clare, Barton, Peter, Braybrooke, Erin, Colclough, Nicola, Dong, Zhiqiang, Evans, Laura, Floc’h, Nicolas, Guérot, Carine, Hargreaves, David, Khurana, Puneet, Li, Songlei, Li, Xiuwei, Lister, Andrew, McCoull, William, McWilliams, Lisa, Orme, Jonathan P., Packer, Martin J., Swaih, Aisha M., Ward, Richard A., Winlow, Poppy, Ye, Yang

“…Herein, we report the identification and optimization of a series of potent inhibitors of EGFR Exon20 insertions with significant selectivity over wild-type…”
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An Investigation into the Prediction of the Plasma Concentration-Time Profile and Its Interindividual Variability for a Range of Flavin-Containing Monooxygenase Substrates Using a Physiologically Based Pharmacokinetic Modeling Approach by Reddy, Venkatesh Pilla, Jones, Barry C, Colclough, Nicola, Srivastava, Abhishek, Wilson, Joanne, Li, Danxi

“…Our recent paper demonstrated the ability to predict in vivo clearance of flavin-containing monooxygenase (FMO) drug substrates using in vitro human hepatocyte…”
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Utilizing microphysiological systems and induced pluripotent stem cells for disease modeling: a case study for blood brain barrier research in a pharmaceutical setting by Fabre, Kristin M., Delsing, Louise, Hicks, Ryan, Colclough, Nicola, Crowther, Damian C., Ewart, Lorna

“…Microphysiological systems (MPS) may be able to provide the pharmaceutical industry models that can reflect human physiological responses to improve drug…”
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Utilizing a Dual Human Transporter MDCKII-MDR1-BCRP Cell Line to Assess Efflux at the Blood Brain Barrier by Colclough, Nicola, Alluri, Ravindra V., Tucker, James W., Gozalpour, Elnaz, Li, Danxi, Du, Hongwen, Li, Wei, Harlfinger, Stephanie, O’Neill, Daniel J., Sproat, Graham G., Chen, Kan, Yan, Yumei, McGinnity, Dermot F.

“…To facilitate the design of drugs readily able to cross the blood brain barrier (BBB), a Madin-Darby canine kidney (MDCK) cell line was established that over…”
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Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of ERK1/2 by Ward, Richard A, Colclough, Nicola, Challinor, Mairi, Debreczeni, Judit E, Eckersley, Kay, Fairley, Gary, Feron, Lyman, Flemington, Vikki, Graham, Mark A, Greenwood, Ryan, Hopcroft, Philip, Howard, Tina D, James, Michael, Jones, Clifford D, Jones, Christopher R, Renshaw, Jonathan, Roberts, Karen, Snow, Lindsay, Tonge, Michael, Yeung, Kay

“…The RAS/RAF/MEK/ERK signaling pathway has been targeted with a number of small molecule inhibitors in oncology clinical development across multiple disease…”
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Unbound Brain-to-Plasma Partition Coefficient, K-p,K-uu,K-brain-a Game Changing Parameter for CNS Drug Discovery and Development by Loryan, Irena, Reichel, Andreas, Feng, Bo, Bundgaard, Christoffer, Shaffer, Christopher, Kalvass, Cory, Bednarczyk, Dallas, Morrison, Denise, Lesuisse, Dominique, Hoppe, Edmund, Terstappen, Georg C., Fischer, Holger, Di, Li, Colclough, Nicola, Summerfield, Scott, Buckley, Stephen T., Maurer, Tristan S., Fridén, Markus

“…Purpose More than 15 years have passed since the first description of the unbound brain-to-plasma partition coefficient (K-p,K-uu,K-brain) by Prof. Margareta…”
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